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2,3-二氢-1H-咪唑并[1,2-b]吡唑对小鼠白血病细胞和正常细胞体内增殖的影响。

Effect of 2,3-dihydro-1 H-imidazo[1,2-b]pyrazole on the proliferation of mouse leukemic and normal cells in vivo.

作者信息

Ganapathi R, Krishan A

出版信息

Cancer Res. 1980 Apr;40(4):1103-8.

PMID:7357541
Abstract

Administration of 2,3-dihydro-1 H-imidazo[1,2-b]pyrazole (IMPY; NSC 51143), 250 to 500 mg/kg, in Day 5 L1210 and P388 (ascites) tumor-bearing mice did not consistently prolong the life span of tumor-bearing animals. Flow cytometry and autoradiographic studies showed that, after 12 to 18 hr of a single IMPY injection, both P388 and L1210 tumor cells were synchronized in S phase. In contrast, IMPY inhibited cellular proliferation in both bone marrow and duodenal crypts during the first 24 hr. and a recovery was detectable only after 36 hr, returning to pretherapy values by 72 hr. Preliminary data indicate that this differential response of normal versus tumor cells to IMPY can be exploited to maximize chemotherapeutic efficacy in scheduled chemotherapy with cycle-specific agents.

摘要

在第5天给L1210和P388(腹水型)荷瘤小鼠注射250至500mg/kg的2,3 - 二氢 - 1H - 咪唑并[1,2 - b]吡唑(IMPY;NSC 51143),并未持续延长荷瘤动物的寿命。流式细胞术和放射自显影研究表明,单次注射IMPY 12至18小时后,P388和L1210肿瘤细胞均同步于S期。相比之下,IMPY在最初24小时内抑制骨髓和十二指肠隐窝中的细胞增殖,仅在36小时后可检测到恢复,到72小时恢复至治疗前值。初步数据表明,正常细胞与肿瘤细胞对IMPY的这种差异反应可用于在使用周期特异性药物的序贯化疗中最大化化疗疗效。

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